Chlorproguanil is a biguanide. Chlorproguanil is active against P. falciparum and P. malariae. Chlorproguanil acts by inhibition of dihydrofolate reductase after cytochrome P450-catalysed cyclization. Chlorproguanil combined with dapsone was developing for the treatment of falciparum malaria. The anti-malarial combination chloroproguanil and dapsone has been withdrawn following demonstration of post-treatment haemolytic anaemia in glucose-6-phosphate dehydrogenase (G6PD) deficient patients in a phase III clinical trial.

Revaprazan (trade name Revanex) is a drug that reduces gastric acid secretion and is used for the treatment of gastritis and acid-related disease. It acts as an acid pump antagonist (potassium-competitive acid blocker) that reversibly inhibits H+, K+-ATPase by binding to the K+-binding site of the pump, thereby causing fewer side effects, compared with the irreversible proton pump inhibitors. Revaprazan is approved for use in Korea, but is not approved in Europe or the United States.

trans-Sobrerol is a mucolytic known due its emplyment in therapy for respiratory diseases. In preclinical studies sobrerol, administered daily at the oral dose of 400 mg/rat, markedly decreased the monocrotaline-induced alterations and regulate the development of pulmonary hypertension. Treatment with sobrerol was well tolerated and significantly reduced frontal headache and rhinorrhoea, efficacy being confirmed by rhinomanometry.

Xylamidine is a peripherally-restricted antagonist of 5HT2A and 5HT1A receptor. It is used to study the role of the serotonin receptors in the regulation of food intake, cardiovascular function, and regulation of body temperature.

Iclaprim is an investigational broad-spectrum diaminopyrimidine antibiotic in development for the treatment of acute bacterial skin and skin structure infections (ABSSSIs). Iclaprim acts on bacterial cells by competitively inhibiting dihydrofolate reductase (DHFR), a key enzyme in the folate cycle; the same mode of inhibition is exerted by trimethoprim. Iclaprim resistance is mainly determined by point mutations in the dfr gene as studied in S. aureus and S. pneumoniae. Surveillance studies demonstrate that the spectrum of activity of iclaprim includes many organisms indicated in cSSSI including S. aureus and S. pyogenes. Iclaprim is bactericidal in vitro, generally at concentrations equal to the MIC that are maintained in human plasma for several hours after a therapeutic dose. Bactericidal activity is primarily time-dependent and concentration independent. Due to its structural similarity with trimethoprim, iclaprim is synergistic with sulfonamides against a broad spectrum of bacterial species. The antimicrobial mechanism of action of iclaprim is mediated by competitive inhibition of bacterial DHFR, the same mode of inhibition exerted by TMP. The activity of iclaprim against TMP-R mutants of S. aureus and S. pneumoniae is attributable to additional hydrophobic interaction between iclaprim and the enzyme. The same mechanism of action of iclaprim, competitive inhibition with the natural substrate DHF, is seen against both TMP-S and -R enzymes. Iclaprim is well suited for use as a first-line empiric monotherapy in patients with ABSSSI who are comorbid with renal impairment for the following reasons. n July 2015, the U.S. Food and Drug Administration, or FDA, designated the IV formulation of iclaprim as a Qualified Infectious Disease Product (QIDP) for ABSSSI and HABP. QIDP status grants iclaprim regulatory Fast Track designation, Priority Review and, if approved, a five-year extension to the statutory market exclusivity period in the United States, resulting in 10 years of market exclusivity from the date of approval.

Mepindolol is a selective beta1-adrenoreceptor blocker with intrinsic sympathetic activity. Treatment with mepindolol dose not significantly affect the lipid levels - the total cholesterol in plasma was decreased by mepindolol but HDL-cholesterol increased. During beta-receptor blockade with mepindolol-sulfate angina was compensated, the unfavourable hemodynamic effects seen during placebo did not occur. No signs of congestive heart failure were found during mepindolol-sulfate-therapy. Mepindolol-sulfate showed a pronounced blood-pressure lowering effect.

Hexacarbacholine is a long-acting muscle-relaxant drug that had been used extensively in Europe in surgical anesthesia, but had had considerably less clinical usage in US. There is no precise agreement concerning the mode of action of hexacarbacholine at the myoneural junction. Therapeutic doses of the drug do not appear to influence the cardiovascular system, cardiac activity, or blood pressure, although large doses do cause slight and transient increases in blood pressure in laboratory animals. The intraocular tension in man is increased temporarily following the administration of hexacarbacholine. Since hexacarbacholine is a cumulative drug, repeated administrations should be avoided. It may cause cardiac arrest due to a hyperkalaemia.

Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.

Fenpiverinium is a quaternary ammonium compound, it is an anticholinergic and antispasmodic agent. It is a constituent of Baralgin. The effects of the constituents of Baralgin (metamizole , fenpiverinium, and pitofenone ) on mechanical activity were studied in isolated human preparations of the upper urinary tract. Fenpiverinium blocked the increase in frequency of phasic-rhythmic contractions and the tonic tension development induced by acetylcholine. Fenpiverinium did influence neither spontaneous phasic activity nor activation by high potassium or norepinephrine. Fenpiverinium has exclusively anticholinergic properties. Fenpiverinium is a muscarinic acetylcholine receptor antagonist.